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Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Carbohydrate Research | Year: 2012

In the present study, carboxymethyl chitosan was prepared from chitosan, crosslinked with glutaraldehyde and evaluated in vitro as a potential carrier for colon targeted drug delivery of ornidazole. Ornidazole was incorporated at the time of crosslinking of carboxymethyl chitosan. The chitosan was evaluated for its degree of deacetylation (DD) and average molecular weight; which were found to be 84.6% and 3.5 × 10 4 Da, respectively. The degree of substitution on prepared carboxymethyl chitosan was found to be 0.68. All hydrogel formulations showed more than 85% and 74% yield and drug loading, respectively. The swelling behaviour of prepared hydrogels checked in different pH values, 1.2, 6.8 and 7.4, indicated pH responsive swelling characteristic with very less swelling at pH 1.2 and quick swelling at pH 6.8 followed by linear swelling at pH 7.4 with slight increase. In vitro release profile was carried out at the same conditions as in swelling and drug release was found to be dependant on swelling of hydrogels and showed biphasic release pattern with non-fickian diffusion kinetics at higher pH. The carboxymethylation of chitosan, entrapment of drug and its interaction in prepared hydrogels were checked by FTIR, 1H NMR, DSC and p-XRD studies, which confirmed formation of carboxymethyl chitosan from chitosan and absence of any significant chemical change in ornidazole after being entrapped in crosslinked hydrogel formulations. The surface morphology of formulation S6 checked before and after dissolution, revealed open channel like pores formation after dissolution. © 2011 Elsevier Ltd. All rights reserved. 26.

Patel M.M.,Kalol Institute of Pharmacy
Research Journal of Pharmaceutical, Biological and Chemical Sciences | Year: 2011

The present study involves screening of different extract of leaves of Grewia asiatica, for hypoglycemic activity on alloxan induced diabetic Wister rats using glibenclamide as standard. Ethanol extracts (200mg/kg b.w. p.o.) shown more significant (p<0.01) reduction in blood glucose level in alloxan induced diabetic Wister rats compared to control and glibenclamide as standard (10 mg/kg b.w. p.o.). And all extracts also screen for phytochemical study revealed presence of Triterpenoids, Alkaloids, Flavonoids, Sterols, Tannins, and Fats as principal chemical constituent.

Patel R.B.,Ganpat University | Patel G.N.,Ganpat University | Patel H.R.,Ganpat University | Patel M.M.,Ganpat University | Patel M.M.,Kalol Institute of Pharmacy
Drug Development and Industrial Pharmacy | Year: 2011

The goal of diabetes therapy today is to achieve and maintain as near normal glycemia as possible to prevent the long-term microvascular and macrovascular complications of an elevated blood glucose. A newly developed inlay osmotic pump tablet (IOPT) can deliver glipizide (GLZ) and metformin HCl (MET) gradually in controlled manner. The aim of present investigation was to prepare the IOPT that can deliver >75% of GLZ in 2h, whereas MET released after 2h and sustained up to 12h. In the present work, HP-β-CD was used to modify the solubility of GLZ before incorporating in the osmotic system and MET was spray-dried with HPMC A15C to modify its release profile, flow property, and compressibility. Various parameters mainly G 75% (75% GLZ release), t LMET (lag time of MET release from device), Q 10 h (percent of MET released within 10h), and RSQ ZERO (R 2 of release data fitted to zero-order equation) were used to compare different formulations. The effects of different formulation variables, that is, osmagents, concentration of hydrophilic polymer, diameter of drug releasing orifice, and coating composition on the drug release profile were investigated. The release rate of GLZ could be effectively modified by the addition of sodium carbonate and sodium chloride, whereas the release rate of MET was adjusted by dual-coating system and by addition of hydrophilic polymer. The developed inlay osmotic system could be effective in the multidrug therapy of diabetes by delivering both drugs in a controlled manner. © 2011 Informa Healthcare USA, Inc.

Shah R.J.,Kalol Institute of Pharmacy | Modi N.R.,Ganpat University | Patel M.J.,Ganpat University | Patel L.J.,Ganpat University | And 2 more authors.
Medicinal Chemistry Research | Year: 2011

The present study deals with the synthesis of novel spiro[azetidine-2,30- indole]-20,4(10H)-dione derivative from the reactions of 3-(phenylimino)-1,3- dihydro-2Hindol- 2-one derivatives with chloracetyl chloride in the presence of triethylamine (TEA). All the compounds were characterized using IR, 1H-NMR, MS, and elemental analysis. They were screened for their antibacterial and antifungal activities. The bacterial strains used were Grampositive Staphylococcus aureus (MTCC-96) and Gramnegative Escherichia coli (MTCC-521) and Pseudomonas aeruginosa (MTCC-647). The antifungal screening was done on Candida albicans (MTCC-183) and Asperigillus niger (MTCC-343) fungal strains. Results revealed that, compounds (7a), (7b), (7c), (7d), and (7e) showed very good activity with MIC value of 6.25-12.5 lg/ml against three evaluated bacterial strains and the remaining compounds showed good to moderate activity comparable to standard drugs as antibacterial agents. Compounds (7c) and (7h) displayed equipotent antifungal activity in comparison to standard drugs. Amoxicillin, gentamycin, and streptomycin were used as standard drugs for antibacterial activity while fluconazole and itraconazole were used as standard drugs for antifungal activity. Structure-activity relationship study of the compounds showed that the presence of electron withdrawing group substitution at 50 and 70 positions of indoline ring and on ortho or para position of phenyl ring increases both antibacterial and antifungal activity of the compound. Henceforth, our findings will have a good impact on chemists and biochemists for further investigations in search of spiro-fused antimicrobial agents. © Springer Science+Business Media, LLC 2011.

Modi N.R.,Smt N M Padalia Pharmacy College | Shah R.J.,Kalol Institute of Pharmacy | Patel M.J.,Ganpat University | Suthar M.,Ganpat University | And 2 more authors.
Medicinal Chemistry Research | Year: 2011

This study deals with the synthesis of novel 2- (2,3-dioxo-2,3-dihydro-1H- indol-1-yl)-N-phenylacetamide derivatives (6a-j) from isatin (3) and 5,7-dibromoisatin (4). All newly synthesized compounds were characterized using IR, 1H NMR, MS, and elemental analysis followed by evaluation of their cytotoxic activity by XTT assay on breast cancer cell line MCF-7 and non-cancer African green monkey cell line VERO. Correlation study for QSAR and in vitro assay was performed. The outcomes indicated that electron withdrawing substitutions at para position of phenyl ring and 5, 7 positions of isatin ring and increasing lipophilicity of the compound increased the cytotoxic activity. The 2-(5,7-dibromo-2,3-dioxo-2,3-dihydro-1H-indol-1-yl)- N-(4-nitrophenyl)acetamide (6b) was found to be the most active compound in the series and demonstrated higher selectivity toward MCF-7 cell line. The IC50 values were 1.96 and 1.90 lM for test compound (6b) and vinblastin (reference drug), respectively. This indicates compound (6b) may possess equipotent cytotoxic activity to vinblastine. The compound (6b) is particularly promising, since it could kill cancer cells 19-20 times more effectively than the non-cancer cells. This property of (6b) may enable us to effectively control tumors with low side effects. Hence, we propose that 2-(5,7-dibromo-2,3-dioxo-2,3-dihydro-1Hindol- 1-yl)-N-(4-nitrophenyl)acetamide may be used as lead for further development. © Springer Science+Business Media, LLC 2010.

Patel D.R.,Kalol Institute Of Pharmacy | Mashru R.C.,M. S. University of Baroda
International Journal of Pharmacy and Technology | Year: 2011

The enantiomeric separation of Bisoprolol fumarate into its enantiomers was achieved by TLC and HPTLC on silica gel plate using optically pure (+)-10-camphorsulphonic acid as a chiral selector in mobile phase and triethyl amine-methanol-1-pentanol (0.14:9.9:0.18, v/v/v) as the solvent system. Spots were located in UV chamber. The detection limit was 8 μg for TLC and 50 ng for HPTLC for both the isomers. The effect of concentration of chiral selector on separation has been studied and satisfactory results were obtained followed by frequent resolution of the enantiomers using these techniques. The procedure was applied successfully to resolve commercially available formulation of bisoprolol fumarate.

Patel D.R.,Kalol Institute of Pharmacy | Patel L.J.,Gujarat University | Patel M.M.,Kalol Institute of Pharmacy
International Journal of ChemTech Research | Year: 2011

A stability-indicating HPLC method has been developed and validated for Repaglinide in bulk drug and pharmaceutical dosage forms. An isocratic RP-HPLC was achieved on younglin HPLC system using Varian C18 (250 × 4.6 mm i.d, 5 μm particle size) column with the mobile phase containing mixture of acetonitrile:10m M ammonium acetate(pH 3.0, adjusted with phosphoric acid) (70: 30, v/v). The flow rate was 1.0ml/min and the eluent was monitored at 230nm. Linearity was found in the range of 0.5-3μg/ml. The values obtained of LODs and LOQs were 0.056μg/ml and 0.172μg/ml respectively. The stress testing of Repaglinide was carried out under acidic, alkaline, oxidative and thermal conditions. Repaglinide was well resolved from its degradation products. The proposed method was validated as per ICH guidelines. The method was found to be fast, accurate, precise, reproducible and suitable for analysis of Repaglinide in bulk and pharmaceutical dosage forms as well as the stability-indicating studies.

Vaghani S.S.,Jodhpur National University | Patel M.M.,Kalol Institute of Pharmacy
Drug Development and Industrial Pharmacy | Year: 2011

The aim of this study was to develop a pH-sensitive chitosan/polyvinyl pyrrolidone (PVP) based controlled drug release system for clarithromycin. The hydrogels were synthesized by cross-linking chitosan and PVP blend with glutaraldehyde to form a semi-interpenetrating polymer network (semi-IPN). These semi-IPNs were studied for their content uniformity, swelling index (SI), mucoadhesion, wettability, in vitro release and their release kinetics. The hydrogels showed more than 97% content of clarithromycin. These hydrogels showed high swelling and mucoadhesion under acidic conditions. The swelling may be due to the protonation of a primary amino group on chitosan. In acidic condition, chitosan would be ionized, and adhesion could have occurred between the positively charged chitosan and the negatively charged mucus. In the alkaline condition, less swelling and mucoadhesion was noticed. In vitro release study revealed that formulation containing chitosan (2% w/v) and PVP (4% w/v) in the ratio of 21:4 showed complete drug release after 12h. Release profile showed that all the formulations followed non-Fickian diffusion mechanism. The cross-linking and compatibility of clarithromycin in the formulation was studied by Fourier transform infrared (FTIR) spectroscopic analysis, differential scanning calorimetry (DSC) and powder X-ray diffraction (p-XRD) study, which confirmed proper formation of semi-IPN and stability of clarithromycin in the formulations. The surface morphology of semi-IPN was studied before and after dissolution in simulated gastric fluid (SGF, pH 1.2) which revealed pores formation in membrane after dissolution. The results of study suggest that semi-IPNs of chitosan/PVP are potent candidates for delivery of clarithromycin in acidic environment. © 2011 Informa Healthcare USA, Inc.

Patel D.B.,Nootan pharmacy college | Patel M.M.,Kalol institute of pharmacy
International Journal of Pharma and Bio Sciences | Year: 2010

Mucoadhesive tablets of diltiazem hydrochloride were formulated as matrix tablets employing, polyethylene oxide (Polyox) and hydroxypropylmethylcellulose (HPMC) and were investigated for mucoadhesion and drug release behavior. Tablets formulated using different viscosity grades of Polyox showed the drug release decreased with viscosity of Polyox increased. Tablet prepared with Polyox alone were slowly eroded and were dissolved completely within 6-10 hours. The mucoadhesive strength of the matrices increased with increase in polymer content. When HPMC was incorporated, the tablets remained intact and provided slow release of diltiazem for over 12 hr. A 3 2 full factorial design was conducted to optimized the formulation. The kinetic modeling study of all batches was shown anomalous pattern of drug release. The drug was released by both erosion and diffusion mechanism. Thus the developed formulation can be suitable for targeted delivery of diltiazem in upper part of GI tract where the absorption of diltiazem is more confined.

Patel J.J.,Kalol Institute of Pharmacy | Acharya S.R.,Nirma University | Acharya N.S.,Nirma University
Journal of Ethnopharmacology | Year: 2014

Ethnopharmacological relevance Clerodendrum serratum (L.) Moon. (Verbenaceae) is an important medicinal plant growing in the tropical and warm temperate regions like Africa, Southern Asia; Malaysia and distributed throughout in forests of India and Sri Lanka. It is traditionally valued and reported for treating pain, inflammation, rheumatism, respiratory disorders, fever and malarial fever in India with a long history. To provide a comprehensive overview of the traditional and ethno medicinal uses, phytochemistry and biological activities of C. serratum with clinical and toxicity data and possibly make recommendations for further research. Materials and methods All relevant worldwide accepted databases were searched for the terms "Clerodendrum", "Clerodendrum serratum", "Bharangi" and "Cheruthekku" along with the other literature from Indian classical texts and pharmacopoeias. There was no specific timeline set for the search. The accessible literatures available on C. serratum were collected via electronic search using Pubmed, Scopus, Science Direct and traditional books reports on ethnopharmacology and traditional medicines. Results C. serratum has played an important role in Indian system of medicine. In addition to the common local use in respiratory diseases, other ethnomedicinal uses include treatment of pain, inflammation, rheumatism and fever especially malarial fever. Scientific studies on extracts and formulations revealed anti-asthmatic, mast cell stabilization and anti-allergic effects of roots of C. serratum. Reported data on pharmacological activities also includes hepatoprotective, anti-oxidant, anti-inflammatory and anticancer potential of the drug. Saponins (terpenoids and steroids), flavonoids and phenolics isolated from roots have been the focus of phytochemical investigations as the biological activity has been ascribed to the saponins, which are known to possess anti-inflammatory and anti-cancer activity. Isolated bioactives from roots like icosahydropicenic acid and ursolic acid have been claimed to offer anti-allergic and hepatoprotective activity. Conclusions Therapeutic potential of roots and leaves of C. serratum has been demonstrated in the conditions like asthma, allergy, fever, inflammation and liver disorders attributed to the presence of various flavonoids, phenolics and saponins present in the drug. Many ethnobotanical claims have been confirmed through modern in-vitro and in-vivo pharmacological studies of different extracts and isolates from plant; however, additional studies on the biomarkers are needed to establish mechanism of action and to validate the traditional use of this drug in clinical practices after proper safety assessment. © 2014 Elsevier Ireland Ltd. All rights reserved.

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